2. Signaling Pathways
  3. Metabolic Enzyme/Protease
  4. Cathepsin

Cathepsin

Cathepsin

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Cathepsins are protease enzymes, categorized into multiple families. Cathepsins can be serine protease, cysteine protease, or aspartyl protease. There are about 15 classes of cathepsins in humans (Cathepsin A, B, C, D, E, F, G, H, K, L, O, S, V, W, and Z). Cathepsins are active in the low pH milieu of lysosomes and are versatile in their functions. Like other enzymes, they are vital for the normal physiological functions such as digestion, blood coagulation, bone resorption, ion channel activity, innate immunity, complement activation, apoptosis, vesicular trafficking, autophagy, angiogenesis, proliferation, and metastasis, among scores of others.

Numerous pathologies have been attributed to the dysregulated cathepsins, some of which include arthritis, periodontitis, pancreatitis, macular degeneration, muscular dystrophy, atherosclerosis, obesity, stroke, Alzheimer's disease, schizophrenia, tuberculosis, and Ebola.

Cathepsin Isoform Specific Products:

Cathepsin Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-146581
    Cathepsin C-IN-4
    		Inhibitor
    Cathepsin C-IN-4 (compound SF27) is a potent Cathepsin C (Cat C) inhibitor, with an IC50 of 65.6 nM. Cathepsin C-IN-4 also inhibits THP-1 and U937 cell, with IC50 values of 203.4 and 177.6 nM, respectively.
    Cathepsin C-IN-4
  • HY-144812
    Gü1303
    		Inhibitor
    Gü1303 is a potent, reversible, slow-binding cathepsin K (CatK) inhibitor with a Ki of 0.91 nM for mature CatK (mCatK). Gü1303 suppresses the autocatalytic activation of the cathepsin K zymogen.
    Gü1303
  • HY-161342
    CTSL/CAPN1-IN-2
    		Inhibitor
    CTSL/CAPN1-IN-2 (Compound 14b) is an orally active inhibitor of both CTSL and CAPN1, with IC50 values of 6.88 nM and 347.6 nM, respectively. CTSL/CAPN1-IN-2 possesses anti-inflammatory properties and favorable pharmacokinetic characteristics. CTSL/CAPN1-IN-2 exhibits broad-spectrum antiviral activity against coronaviruses by blocking viral entry.
    CTSL/CAPN1-IN-2
  • HY-123531
    JNJ 10329670
    		Inhibitor
    JNJ 10329670 is a potent and selective noncovalent cathepsin S inhibitor with a Ki value of 34 nM for human cathepsin S. JNJ 10329670 blocks invariant chain proteolysis in B cells and dendritic cells, as well as antigen-induced T cell proliferation.
    JNJ 10329670
  • HY-151524
    Cathepsin K inhibitor 3
    		Inhibitor
    Cathepsin K inhibitor 3 (compound 23) is a highly selective cathepsin K inhibitor with an IC50 value of 0.5 nM. Cathepsin K inhibitor 3 has a favorable pharmacokinetic profile and may be used in osteoarthritis (OA) disease studies.
    Cathepsin K inhibitor 3
  • HY-D1634A
    Bz-FVR-AMC TFA
    Bz-FVR-AMC TFA is a fluorogenic substrate for procathepsin with a kcat/Km value of 1070 mM-1s-1. The high concentration of BZ-FVR-AMC inhibits the substrate.
    Bz-FVR-AMC TFA
  • HY-D1523
    Z-Arg-Arg-4MβNA triacetate
    Z-Arg-Arg-4MβNA triacetate is a cathepsin B-specific substrate and can produce fluorescent end product 4MβNA (λex = 355 nm, λem = 430 nm).
    Z-Arg-Arg-4MβNA triacetate
  • HY-P10118
    Cathepsin L-IN-3
    		Inhibitor
    Cathepsin L-IN-3 is a tripeptide-sized cathepsin L inhibitor.
    Cathepsin L-IN-3
  • HY-W796158
    Z-DEVD-CMK
    		Inhibitor
    Z-DEVD-CMK is an irreversible inhibitor of most of the cathepsins in vitro.
    Z-DEVD-CMK
  • HY-122161
    JNJ-10311795
    		Inhibitor
    JNJ-10311795 (RWJ-355871), a potent dual inhibitor of neutrophil cathepsin G (Ki = 38 nM) and mast cell chymase (Ki = 2.3 nM), exhibits noteworthy antiinflammatory activity.
    JNJ-10311795
  • HY-P4500
    Z-Arg-Arg-pNA
    Z-Arg-Arg-pNA is a substrate for cathepsin B and can be used to detect this enzyme activity.
    Z-Arg-Arg-pNA
  • HY-152204
    Cathepsin L/S-IN-1
    		Inhibitor
    Cathepsin L/S-IN-1 is a dual inhibitor of Cathepsin L and Cathepsin S with IC50s of 4.10 μM and 1.79 μM, respectively. Cathepsin L/S-IN-1 shows a significant antimetastatic and invasive effects on pancreatic cancer BxPC-3 and PANC-1 cells.
    Cathepsin L/S-IN-1
  • HY-139685
    ABP 25
    		Inhibitor
    ABP 25 is an activity-based probe for cathepsin K imaging with excellent potency and selectivity.
    ABP 25
  • HY-137392
    Cathepsin L-IN-4
    Cathepsin L-IN-4 is an inhibitor of cathepsin L with IC50 at nanomolar concentrations.
    Cathepsin L-IN-4
  • HY-162477
    TS-24
    		Inhibitor 98.96%
    TS-24 is an inhibitor for cathepsin S, with an IC50 of 4.3 μM. TS-24 exhibits radiosensitizing activity in wild type breast cancer susceptibility gene 1 (BRCA1) and in TNBC xenograft mice model, through induction of apoptosis.
    TS-24
  • HY-108137A
    Z-L(D-Val)G-CHN2
    		Inhibitor 99.35%
    Z-L(D-Val)G-CHN2 is the isoform of Z-LVG-CHN2 (HY-108137). Z-LVG-CHN2 is a cell-permeable and irreversible inhibitor of cysteine proteinase. Z-LVG-CHN2 is a tripeptide derivative and mimics part of the human cysteine proteinase-binding center. Z-LVG-CHN2 displays an inhibition on HSV whereas no significant effect on poliovirus replication. Z-LVG-CHN2 effectively blocks SARS-COV-2 replication (EC50=190 nM) via inhibition of SARS-COV-2 3CL pro protease.
    Z-L(D-Val)G-CHN2
  • HY-119293A
    K777 tosylate
    		Inhibitor
    K777 tosylate is a potent, orally active and irreversible cysteine protease inhibitor. K777 tosylate is also a potent CYP3A4 inhibitor with an IC50 of 60 nM and a selective CCR4 antagonist featuring the potent chemotaxis inhibition. K777 tosylate irreversibly inhibits Cruzain, the major cysteine protease of Trypansoma cruzi, and cathepsins B and L. K777 tosylate is a broad-spectrum antiviral by targeting cathepsin-mediated cell entry. K777 tosylate inhibits SARS-CoV and EBOV pseudovirus entry with IC50 values of 0.68 nM and 0.87 nM, respectively.
    K777 tosylate
  • HY-P5975
    Z-Leu-Leu-Leu-fluoromethyl ketone
    		Inhibitor
    Z-Leu-Leu-Leu-fluoromethyl ketone (Z-LLL-FMK) is a cysteine protease inhibitor. Z-Leu-Leu-Leu-fluoromethyl ketone inhibits SARS infection. Z-Leu-Leu-Leu-fluoromethyl ketone also protects mice against a T. crassiceps challenge.
    Z-Leu-Leu-Leu-fluoromethyl ketone
  • HY-115454
    GB111-NH2
    		Inhibitor
    GB111-NH2 is a cysteine cathepsin inhibitor and can be used in cancer research.
    GB111-NH2
  • HY-153614
    Ac-VLPE-FMK
    		Inhibitor ≥99.0%
    Ac-VLPE-FMK, a tetrapeptidyl mono-fluoromethyl ketone (m-FMK), is a Cat-B and Cat-L inhibitor. Ac-VLPE-FMK can be used for the research of cancer aggressiveness.
    Ac-VLPE-FMK
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Cathepsin Isoform Comparison

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